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Assay Detail

CHEMBL798016

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity against RXR alpha receptor using [3H]9-cis-RA as radioligand in CV-1 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cercopithecidae
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Retinoic acid receptor RXR-alpha (CHEMBL2061)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Michellys PY, Boehm MF, Chen JH, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Yumibe N, Ardecky RJ.
Bioorg Med Chem Lett (2003) 13 : 4071 -4075
PubMed 14592510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.28 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL133915 1 9.10
CHEMBL130374 1 9.10
CHEMBL130232 1 9.00
CHEMBL42314 1 8.82
CHEMBL422088 1 8.64
CHEMBL337393 1 8.59
CHEMBL130317 1 8.52
CHEMBL335242 1 8.39
CHEMBL131826 1 8.36
CHEMBL424639 1 8.21
CHEMBL133896 1 8.20
CHEMBL111217 1 8.11
CHEMBL288436 1 7.89
CHEMBL424269 1 7.67
CHEMBL132568 1 7.59
CHEMBL130231 1 7.54
CHEMBL131122 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL133915 Ki = 0.8 nM 9.10
CHEMBL130374 Ki = 0.8 nM 9.10
CHEMBL130232 Ki = 1.0 nM 9.00
CHEMBL42314 Ki = 1.5 nM 8.82
CHEMBL422088 Ki = 2.3 nM 8.64
CHEMBL337393 Ki = 2.6 nM 8.59
CHEMBL130317 Ki = 3.0 nM 8.52
CHEMBL335242 Ki = 4.1 nM 8.39
CHEMBL131826 Ki = 4.4 nM 8.36
CHEMBL424639 Ki = 6.1 nM 8.21
CHEMBL133896 Ki = 6.3 nM 8.20
CHEMBL111217 Ki = 7.8 nM 8.11
CHEMBL288436 Ki = 12.9 nM 7.89
CHEMBL424269 Ki = 21.4 nM 7.67
CHEMBL132568 Ki = 25.6 nM 7.59
CHEMBL130231 Ki = 28.7 nM 7.54
CHEMBL131122 Ki = 85.8 nM 7.07